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Chemical Structure| 727699-84-5 同义名 : -
CAS号 : 727699-84-5
货号 : A994632
分子式 : C26H21FN2O4S
纯度 : 95%
分子量 : 476.519
MDL号 : MFCD04617604
存储条件：

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(524.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The cGAS-STING signalling axis, comprising the synthase for the second messenger cyclic GMP-AMP (cGAS) and the cyclic GMP-AMP receptor stimulator of interferon genes (STING), detects pathogenic DNA to trigger an innate immune reaction involving a strong type I interferon response against microbial infections[1]. The cGAS-STING pathway responds to viral, bacterial, and self-DNA. Whereas it generally mediates immune surveillance and is often neuroprotective, excessive engagement of the system can be deleterious[2]. STING-deficient mice exhibited unaltered initial development of HCC, but had higher number of large tumors at late stages of disease. In the liver of STING-deficient HCC mice, we observed reduced levels of phospho-STAT1, autophagy, and cleaved caspase3. These responses were activated in the liver by treatment with a cyclic dinucleotide (CDN) STING agonist. Importantly, CDN treatment of mice after HCC development efficiently reduced tumor size[3]. STING and IRF3 were upregulated in livers of HFD-fed mice and in FFA-induced L-O2 cells. Knocking down either STING or IRF3 led to a significant reduction in FFA-induced hepatic inflammation and apoptosis, as evidenced by modulation of the nuclear factor κB (NF-κB) signaling pathway, inflammatory cytokines, and apoptotic signaling. Additionally, STING/IRF3 knockdown enhanced glycogen storage and alleviated lipid accumulation, which were found to be associated with increased expression of hepatic enzymes in glycolysis and lipid catabolism, and attenuated expression of hepatic enzymes in gluconeogenesis and lipid synthesis. GUN35901 is a demethyl analogue of DUN99845. GUN35901 is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.49mL

2.10mL

1.05mL

20.99mL

4.20mL

2.10mL
参考文献

[1] Karl-Peter Hopfner,Veit Hornung. Molecular mechanisms and cellular functions of cGAS-STING signalling. Nat Rev Mol Cell Biol. 2020 Sep;21(9):501-521.

[2]Bindu D Paul,et al. Signaling by cGAS-STING in Neurodegeneration, Neuroinflammation, and Aging. Trends Neurosci. 2021 Feb;44(2):83-96.

[3]Martin K Thomsen,et al. The cGAS-STING pathway is a therapeutic target in a preclinical model of hepatocellular carcinoma. Oncogene. 2020 Feb;39(8):1652-1664.

[4]J T Qiao,et al. Activation of the STING-IRF3 pathway promotes hepatocyte inflammation, apoptosis and induces metabolic disorders in nonalcoholic fatty liver disease. Metabolism. 2018 Apr;81:13-24.